公开(公告)号：US20120046267A1

公开(公告)日：2012-02-23

申请号：US13025281

申请日：2011-02-11

Applicant: Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

Inventor： Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

IPC: A61K31/4355 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/5377 ,  C07D495/04 ,  A61K31/4365 ,  A61K31/519 ,  A61K31/5025 ,  C07D513/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/502 ,  C12N9/99 ,  A61P35/00 ,  A61P29/00 ,  C07D491/048

CPC classification number: C07D491/048

Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.

Abstract translation: 式1的化合物，如下文所定义：其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分由TAK1驱动的肿瘤，或适合于 TAK1抑制剂有效。 本发明并不限于本发明。

公开(公告)号：US20090286768A1

公开(公告)日：2009-11-19

申请号：US12468188

申请日：2009-05-19

Applicant: Andrew P. Crew ,  Meizhong Jin ,  Mridula Kadalbajoo ,  Andrew Kleinberg ,  Mark J. Mulvihill ,  Jing Wang

Inventor： Andrew P. Crew ,  Meizhong Jin ,  Mridula Kadalbajoo ,  Andrew Kleinberg ,  Mark J. Mulvihill ,  Jing Wang

IPC: A61K31/4985 ,  C07D487/04 ,  A61K31/53

CPC classification number: C07D487/04

Abstract: Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.

Abstract translation: 具有本文所定义的结构式I的结构的基于吡啶的双环化合物，其药学上可接受的盐，其制备，组合物和疾病治疗。 本摘要不限定或限制本发明。

公开(公告)号：US08735405B2

公开(公告)日：2014-05-27

申请号：US13446629

申请日：2012-04-13

Applicant: Lee D. Arnold ,  Cara Cesario ,  Heather Coate ,  Andrew P. Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark J. Mulvihill ,  Anthony I. Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Yingchuan Sun ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang

Inventor： Lee D. Arnold ,  Cara Cesario ,  Heather Coate ,  Andrew P. Crew ,  Hanqing Dong ,  Kenneth Foreman ,  Ayako Honda ,  Radoslaw Laufer ,  An-Hu Li ,  Kristen Michelle Mulvihill ,  Mark J. Mulvihill ,  Anthony I. Nigro ,  Bijoy Panicker ,  Arno G. Steinig ,  Yingchuan Sun ,  Quinghua Weng ,  Douglas S. Werner ,  Michael J. Wyle ,  Tao Zhang

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07F5/025 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

Abstract translation: 其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，R 1和Q 1在本文中定义的式及其药学上可接受的盐的化合物抑制IGF-1R酶，并且可用于治疗和/或预防 过度增生性疾病如癌症，炎症，牛皮癣，过敏/哮喘，免疫系统的疾病和状况，中枢神经系统的疾病和状况。

公开(公告)号：US08399433B2

公开(公告)日：2013-03-19

申请号：US12791047

申请日：2010-06-01

Applicant: Rama Devi Appari ,  Xin Chen ,  Ramesh Chilukuri ,  Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Kenneth Foreman ,  Ramesh C. Gupta ,  An-Hu Li ,  Dan Sherman ,  Kathryn M. Stolz ,  Brian Volk ,  Robert Zahler

Inventor： Rama Devi Appari ,  Xin Chen ,  Ramesh Chilukuri ,  Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Kenneth Foreman ,  Ramesh C. Gupta ,  An-Hu Li ,  Dan Sherman ,  Kathryn M. Stolz ,  Brian Volk ,  Robert Zahler

IPC: A61K31/675 ,  C07D279/10 ,  C07D413/12 ,  C07F9/08

CPC classification number: C07F9/65583 ,  A61K31/497 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07F9/6512 ,  C07F9/6544

Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.

公开(公告)号：US20130261086A1

公开(公告)日：2013-10-03

申请号：US13990045

申请日：2011-11-29

Applicant: Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

Inventor： Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

IPC: C07F9/6584

CPC classification number: C07F9/6584 ,  A61K31/675

Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.

Abstract translation: 式（I）化合物：其中变量在本文中定义，以及其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括FAK抑制有益的癌症。

公开(公告)号：US08378104B2

公开(公告)日：2013-02-19

申请号：US13025281

申请日：2011-02-11

Applicant: Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

Inventor： Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

IPC: C07D471/02

CPC classification number: C07D491/048

Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.

Abstract translation: 式1的化合物，如下文所定义：其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分由TAK1驱动的肿瘤，或适合于 TAK1抑制剂有效。 本发明并不限于本发明。

公开(公告)号：US20110136764A1

公开(公告)日：2011-06-09

申请号：US12791047

申请日：2010-06-01

Applicant: Rama Devi APPARI ,  Xin CHEN ,  Ramesh Chllukuri ,  Andrew P. CREW ,  Hanqing DONG ,  Caterina FERRARO ,  Kenneth FOREMAN ,  Ramesh C. GUPTA ,  An-Hu LI ,  Dan SHERMAN ,  Kathryn M. STOLZ ,  Brian VOLK ,  Robert ZAHLER

Inventor： Rama Devi APPARI ,  Xin CHEN ,  Ramesh Chllukuri ,  Andrew P. CREW ,  Hanqing DONG ,  Caterina FERRARO ,  Kenneth FOREMAN ,  Ramesh C. GUPTA ,  An-Hu LI ,  Dan SHERMAN ,  Kathryn M. STOLZ ,  Brian VOLK ,  Robert ZAHLER

IPC: A61K31/675 ,  C07F9/6558 ,  C07F9/6561 ,  C07F9/6564 ,  A61P35/00

CPC classification number: C07F9/65583 ,  A61K31/497 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07F9/6512 ,  C07F9/6544

Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.

Abstract translation: 合成，中间体，制剂及其治疗方法，包括至少部分由FAK介导的癌症的式1化合物，如下文所定义。

公开(公告)号：US07767673B2

公开(公告)日：2010-08-03

申请号：US12209862

申请日：2008-09-12

Applicant: Arlindo L. Castelhano ,  Andrew P. Crew ,  Han-Qing Dong ,  Radoslaw Laufer ,  An-Hu Li ,  Li Qiu ,  Colin Peter Sambrook Smith ,  Tao Zhang

Inventor： Arlindo L. Castelhano ,  Andrew P. Crew ,  Han-Qing Dong ,  Radoslaw Laufer ,  An-Hu Li ,  Li Qiu ,  Colin Peter Sambrook Smith ,  Tao Zhang

IPC: A61K31/5377 ,  C07D413/12

CPC classification number: C07D471/04

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-Oxide thereof, are useful in the treatment of cancer.

Abstract translation: 由式（I）表示的化合物或其药学上可接受的盐或N-氧化物可用于治疗癌症。

公开(公告)号：US08481733B2

公开(公告)日：2013-07-09

申请号：US12468188

申请日：2009-05-19

Applicant: Andrew P. Crew ,  Meizhong Jin ,  Mridula Kadalbajoo ,  Andrew Kleinberg ,  Mark J. Mulvihill ,  Jing Wang

Inventor： Andrew P. Crew ,  Meizhong Jin ,  Mridula Kadalbajoo ,  Andrew Kleinberg ,  Mark J. Mulvihill ,  Jing Wang

IPC: C07D487/04 ,  C07D403/04 ,  A61K31/4985 ,  A61P11/06

CPC classification number: C07D487/04

Abstract: Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.

Abstract translation: 具有本文所定义的结构式I的结构的基于吡啶的双环化合物，其药学上可接受的盐，其制备，组合物和疾病治疗。 本摘要不限定或限制本发明。

公开(公告)号：US09133224B2

公开(公告)日：2015-09-15

申请号：US13990045

申请日：2011-11-29

Applicant: Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

Inventor： Andrew P. Crew ,  Hanqing Dong ,  Caterina Ferraro ,  Dan Sherman ,  Kam W. Siu

IPC: A61K31/675 ,  C07F9/6584

CPC classification number: C07F9/6584 ,  A61K31/675

Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.

Abstract translation: 式（I）化合物：其中变量在本文中定义，以及其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括FAK抑制有益的癌症。